(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮
| 中文名称 | (2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮 |
|---|---|
| 中文同义词 | (2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮;PPM1D抑制剂(CCT007093);化合物CCT007093 |
| 英文名称 | Cyclopentanone, 2,5-bis(2-thienylMethylene)-, (E,E)- |
| 英文同义词 | (2E,5E)-2,5-Bis(2-thienylmethylene)cyclopentanone CCT007093;Cyclopentanone, 2,5-bis(2-thienylMethylene)-, (E,E)-;CCT007093;(2E,5E)-2,5-Bis(2-thienylmethylene)cyclopentanone;(2E,5E)-2,5-Bis(thiophen-2-ylmethylene)cyclopentanone;2,5-bis(2-thienylMethylene)-, (E,E)-Cyclopentanone;CCTOO7093;2,5-Bis(2-thienylmethylene)-cyclopentanone |
| CAS号 | 176957-55-4 |
| 分子式 | C15H12OS2 |
| 分子量 | 272.39 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂;小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors |
| Mol文件 | 176957-55-4.mol |
| 结构式 |  |
(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮 性质
| 熔点 | 222-223℃ |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：>3mg/mL |
| 形态 | 粉末，黄色 |
| 敏感性 | Light Sensitive |
环戊酮曼尼希碱类化合物是由天然萜类化合物进行结构改造而设计合成的一类具有抗炎活性的化合物。构效关系研究显示二(2-噻吩基亚甲基)环戊酮曼尼希碱类化合物抗炎活性较强。(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮是其中代表性化合物。
以2-噻吩甲醛及环戊酮或N-环戊烯基吗啉为起始物料，经曼尼希反应制备得到目标化合物(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮。其合成反应式如下图：
CCT007093 (25 or 50 µM, 8 h) significantly increases the phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159, and the phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) are also up-regulated in transfected HEK293T cell line.
CCT007093 shows specificity for MCF-7 cells, reducing viability by 40% after 2 days with no observable effect on the growth of HeLa cells.
CCT007093 induces P38 phosphorylation at 4 h post exposure in MCF-7 cells (sensitive to PPM1D inhibition), and does not induce P38 phosphorylation in HeLa cells (relatively resistant to PPM1D inhibition).
Western Blot Analysis
| Cell Line: | HEK293T cell line. |
| Concentration: | 25 or 50 µM. |
| Incubation Time: | 8 h. |
| Result: |
The phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159 were all significantly increased
[1]
.
The phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) were also up-regulated [1] . |
CCT007093 (6.4 mg/kg) enhances liver regeneration and increases the survival rate of mice following major hepatectomy.
| Animal Model: | Wild-type mice. |
| Dosage: | 3.2 and 6.4 mg/kg. |
| Administration: | Injected intraperitoneally 4 times (mice were sacrificed at 36 h post-PH). |
| Result: |
Significantly improved survival in mice following major hepatectomy (80% hepatectomy).
The level of PCNA was also significantly increased in the liver of CCT007093-treated mice at 36h, 48h and 72h post-PH. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15880 | CCT007093 | 5 mg | 400元 | |
| 2024/01/25 | HY-15880 | (2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮 CCT007093 | 176957-55-4 | 10mM * 1mLin DMSO | 440元 |